Synthesis and Evaluation of Colchicine C-Cyclic AmineDerivatives As Potent Anti-Biofilms Agents AgainstMethicillin-Resistant

Overview

Journal Antibiotics (Basel)

Specialty Pharmacology

Date 2025 Feb 26

PMID 40001417

Authors

Yuxin Yang

Xin Liu

Can Sun

Yuan Fang

Danyang Qu

Zhengbin Tang

Zetao Sun

Xiaoping Zhou

Dacheng Wang

Affiliations

Soon will be listed here.

Abstract

Background/objectives: The elimination of bacterial biofilm formation is an effective strategy against bacterial infections. The objective was to design 27 colchicine C-ring modified amine derivatives and evaluate their inhibitory activities against the biofilms of MRSA USA300.

Methods: Design 27 colchicine C-ring modified amine derivatives. Evaluate their inhibitory activities against MRSA USA300 biofilms. Conduct antibacterial or synergistic antibacterial experiments. Research the phenotypic mechanisms related to biofilm-related genes and .

Results: The experiments showed that most compounds in this series exhibited varying degrees of biofilm inhibitory activity (with inhibition rates ranging from 7.72% to 40.79%). Further verification through antibacterial or synergistic antibacterial experiments revealed that the compounds with biofilm-inhibiting effects (compounds ) generally had certain antibacterial activities (MICs = 16-32 μg/mL) or synergistic antibacterial effects (FICIs < 0.5). Furthermore, through in-depth research on their phenotypic mechanisms (i.e., research on biofilm-related mechanisms), it was found that the compounds with antibacterial or synergistic antibacterial properties could inhibit the formation of biofilms by affecting the regulation of the biofilm-related genes and .

Conclusions: The designed colchicine C-ring modified amine derivatives showed potential in inhibiting MRSA biofilms, and their antibacterial or synergistic antibacterial properties are related to the regulation of biofilm-related genes and , demonstrating inhibitory activity against MRSA.

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